Drug intelligence / Profile preview

adinazolam

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Adinazolam is a triazolobenzodiazepine derivative developed in the 1980s by Upjohn as an anxiolytic, anticonvulsant, sedative, and antidepressant. It was designed to enhance the antidepressant effects of alprazolam. Mechanistically, adinazolam acts as a positive allosteric modulator at the GABA(A) receptor benzodiazepine binding site and also binds to peripheral-type benzodiazepine receptors (translocator protein), potentiating GABAergic inhibition in the central nervous system[1][2][3][4]. Its main active metabolite is N-desmethyladinazolam, which has higher affinity for benzodiazepine receptors than its parent compound[6][7]. Although it showed efficacy comparable to imipramine for major depression and had anxiolytic properties in clinical studies, it was never approved by the FDA due to mixed results and concerns about safety or abuse potential[1][3][4]. In recent years, adinazolam has appeared on designer drug markets as a novel psychoactive substance with documented abuse potential and withdrawal symptoms[5].

Brand names
Deracyn
Other names
AdinazolamumAdinazolamum [INN-Latin]Adinazolam [USAN]
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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